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目的制备共载阿霉素(DOX)和维拉帕米(VER)双修饰脂质体[CL-R8-LP(DOX+VER)],考察其对耐药人乳腺癌细胞MCF-7/ADR增殖的抑制作用。方法采用硫酸铵梯度法制备CL-R8-LP(DOX+VER),HPLC法测定其包封率,MTT法测定不同处方制备的脂质体对MCF-7/ADR细胞增殖的抑制作用。结果所制备的CL-R8-LP(DOX+VER)粒径约90 nm,电位接近电中性;DOX和VER的包封率分别为94.96%±1.32%、70.48%±1.45%;与游离DOX和单载DOX的双修饰脂质体[CL-R8-LP(DOX)]相比,CL-R8-LP(DOX+VER)对MCF-7/ADR细胞的增殖有更强的抑制作用。结论CL-R8-LP(DOX+VER)具有治疗耐药人乳腺癌的前景。
Objective To prepare double-modified liposomes (DOX + VER) co-loaded with doxorubicin (DOX) and verapamil (VER) Inhibition of proliferation. Methods CL-R8-LP (DOX + VER) was prepared by ammonium sulfate gradient method. The entrapment efficiency was determined by HPLC. The inhibitory effect of liposomes prepared by different prescriptions on the proliferation of MCF-7 / ADR cells was determined by MTT assay. Results The particle size of CL-R8-LP (DOX + VER) was about 90 nm and the potential was nearly neutral. The entrapment efficiencies of DOX and VER were 94.96% ± 1.32% and 70.48% ± 1.45% CL-R8-LP (DOX + VER) had a stronger inhibitory effect on MCF-7 / ADR cell proliferation than DOX loaded double-modified liposome [CL-R8-LP (DOX)]. Conclusions CL-R8-LP (DOX + VER) has the potential of treating resistant human breast cancer.